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Target intelligence / Profile preview
Melanocortin-4 Receptor (MC4R)
- Target
- MC4R
- Molecular classification
- G protein-coupled receptor, GPCR, Rhodopsin-like Class A GPCR
01
Overview
The melanocortin-4 receptor (MC4R) is a G protein-coupled receptor (GPCR) that plays a central role in regulating energy homeostasis, food intake, and metabolism. It is highly expressed in the paraventricular nucleus of the hypothalamus and is a key component of the leptin-melanocortin pathway. Mutations in MC4R are a common monogenic cause of severe early-onset obesity. Extracellular calcium acts as a cofactor for ligand binding, increasing affinity and potency. MC4R can also couple with ion channels, such as Kir7.1, adding complexity to its signaling modalities.
02
Mechanism of action
Agonists stimulate cAMP production via Gs proteins; antagonists block agonist-mediated activation.
03
Biological functions
Appetite regulationEnergy balanceMetabolismSexual functionSignal transduction
04
Disease associations
Obesity
05
Safety considerations
Variable impact of mutations on receptor activity.Potential for off-target effects due to broad expression in the brain and other tissues.
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